Repaglinide

It is an antidiabetic drug in the class of medications known as meglitinides, and was invented in 1983

Repaglinide

Repaglinide; 135062-02-1; Prandin; NovoNorm; GlucoNorm

Eurepa, Eurepa-MF, Novonorm, Page, Q-Repa, Rapilin, Regan, Repa, Repide, Restrict

2-ethoxy-4-({[(1S)-3-methyl-1-[2-(piperidin-1-yl)phenyl]butyl]carbamoyl}methyl)benzoic acid

>98% protein binding.

Insulin secretion by pancreatic β cells is partly controlled by cellular membrane potential. Membrane potential is regulated through an inverse relationship between the activity of cell membrane ATP-sensitive potassium channels (ABCC8) and extracellular glucose concentrations. By inhibiting ATP-sensitive potassium channels, repaglinide increases insulin release in a glucose-dependent manner.

Usual initial dose: 0.5 mg, taken within 30 minutes of main meals. 

Type 2 diabetes mellitus.

Vomiting, hypoglycaemia, constipation, nausea, arthralgia, diarrhoea, dyspepsia, rhinitis, sinusitis, back pain; rash, pruritus, urticaria; visual disturbances.

• Cytochrome P450 3A4 inducers eg. rifampicin, barbiturates and carbamazepine may increase repaglinide metabolism.
• itraconazole ketoconazole, erythromycin and fluconazole may increase plasma conc of repaglinide.
• Antagonistic effect with drugs causing hyperglycaemia.
• Absorption may be affected when given with food.
• When used with isophane insulin the risk of myocardial infarction increased.

Diabetic ketoacidosis; severe hepatic impairment, type 1 diabetes; hypersensitivity. Lactation.

Store below 25°C. Protect from moisture

Molecular weight

452.5857

Molecular formula

C27H36N2O4

CAS number

135062-02-1

Precautions

• Myocardial infarction
• Malnourished and debilitated patients.
• Trauma during surgery
• Elderly
• Coma
• Pregnancy.
• Hepatic or severe renal impairment.